Nozaki S, Kihara S, Kubo M, Kameda K, Matsuzawa Y, Tarui S
Second Department of Internal Medicine, Osaka University Medical School, Japan.
Int J Clin Pharmacol Ther Toxicol. 1987 Dec;25(12):643-7.
The relation of plasma levels of prostaglandins to the occurrence of flushing induced by niceritrol was investigated. Niceritrol increased plasma levels of PGE2 (p less than 0.01) and 6 keto-PGF1 alpha (p less than 0.05) in 10 male subjects and aspirin reduced the level of PGE2 (p less than 0.01). Five of 10 subjects had flushing, and aspirin reduced flushing in 4 subjects. On the basis of the above study, we treated 35 hyperlipidemic patients with niceritrol in combination with aspirin, investigating the effect of the treatment of serum lipids and postheparin lipolytic activity. None of the 12 cases given aspirin from the start of the treatment experienced flushing, whereas 9 of the 23 cases not given aspirin experienced flushing, which was suppressed by adding aspirin in prescription in all cases except one. Niceritrol decreased serum cholesterol, triglyceride and atherogenic index. It also increased HDL2 cholesterol and decreased HDL3 cholesterol. The LPL activity in postheparin plasma increased in all cases after niceritrol treatment. In conclusion, aspirin increased compliance of niceritrol by reducing the occurrence of flushing probably due to the decreased levels of prostaglandins, yielding favorable results for the long-term treatment of hyperlipidemia with a sufficient doses of niceritrol.
研究了前列腺素血浆水平与硝乙脲引起的脸红之间的关系。在10名男性受试者中，硝乙脲使PGE2血浆水平升高（p<0.01），6-酮-PGF1α血浆水平升高（p<0.05），而阿司匹林降低了PGE2水平（p<0.01）。10名受试者中有5名出现脸红，阿司匹林使4名受试者的脸红减轻。基于上述研究，我们用硝乙脲联合阿司匹林治疗35例高脂血症患者，观察其对血脂及肝素后脂解活性的治疗效果。治疗开始时给予阿司匹林的12例患者均未出现脸红，而未给予阿司匹林的23例患者中有9例出现脸红，除1例外，所有病例在处方中加用阿司匹林后脸红均得到抑制。硝乙脲可降低血清胆固醇、甘油三酯和致动脉粥样硬化指数。它还可升高HDL2胆固醇水平，降低HDL3胆固醇水平。硝乙脲治疗后所有病例肝素后血浆中的LPL活性均升高。总之，阿司匹林可能通过降低前列腺素水平减少脸红的发生，从而提高了硝乙脲的耐受性，为大剂量硝乙脲长期治疗高脂血症带来了良好效果。
